1170069-87-0Relevant articles and documents
Novel 8-arylated purines as inhibitors of glycogen synthase kinase
Ibrahim, Nada,Mouawad, Liliane,Legraverend, Michel
scheme or table, p. 3389 - 3393 (2010/08/06)
A series of 8-arylated purine derivatives bearing either an aniline or an alkyl amide at position 6 were found to inhibit glycogen synthase kinase-3,with good selectivity over ten kinases. Molecular modeling studies indicated that the most active compounds (8a and 8e),adopt a planar conformation,close to the shape of AMPPNP in the crystal structure of GSK-3. These compounds are stabilized by hydrophobic contacts between the 8-aromatic group and the protein adenine pocket and by electrostatic contacts.
